EasySep™小鼠TIL（CD45）正选试剂盒
产品号 #72962_C
视黄醇通路激活剂；激活视黄酸受体(RAR) α
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总览
AM580是一种选择性激活视黄醇受体（RAR）的激动剂，对RARα 的EC₅₀为 0.36 nM，相较于RARβ （EC₅₀= 24.6 nM）和RARγ （EC₅₀= 27.9 nM）具有高度选择性（Bernard et al.)。它是视黄酸（RA）的衍生物，但与RA相比，它对RARα的特异性更强，而RA对RARα、β或γ的选择性较弱(Gianní et al.; Bernard et al.; Kim et al; Rochette-Egly & Germain)。
重编程
·促进体细胞重编程为诱导多能干细胞（Wang et al.）。
分化
·与GSK3β抑制剂CHIR99021一起作用，可诱导人诱导多能干细胞向中间中胚层分化（Araoka et al.）。
癌症研究
·抑制肿瘤细胞增殖和存活信号通路，诱导细胞凋亡，从而抑制小鼠乳腺肿瘤病毒(MMTV)-neu-和MMTV-wnt1诱导的乳腺增生（Lu et al.）。
·抑制MMTV-Myc小鼠的肿瘤生长（Bosch et al.）。
·抑制子宫内膜癌细胞增殖（Cheng et al.）。
·诱导急性早幼粒细胞白血病细胞分化（Gianní et al.）。
细胞类型
癌细胞及细胞系，白血病/淋巴瘤细胞，中胚层，PSC衍生，多能干细胞
种属
人，小鼠，非人灵长类，其他物种，大鼠
应用
分化，重编程
研究领域
癌症，干细胞生物学
CAS 编号
102121-60-8
化学式
C₂₂H₂₅NO₃
纯度
≥98%
通路
视黄醇类
靶点
RAR
产品说明书及文档
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应用领域
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相关材料与文献
技术资料 (2)
文献 (9)
The Role of Specific Retinoid Receptors in Sebocyte Growth and Differentiation in Culture1
Journal of Investigative Dermatology 2000
Abstract
Retinoic acid derivatives (retinoids) exert their pleiotropic effects on cell development through specific nuclear receptors,the retinoic acid receptors and retinoid X receptors. Despite recent progress in understanding the cellular and molecular mechanisms of retinoid activity,it is unknown which of the retinoid receptor pathways are involved in the specific processes of sebocyte growth and development. In this study,we investigated the roles of specific retinoid receptors in sebocyte growth and differentiation,by testing the effects of selective retinoic acid receptor and retinoid X receptor ligands at concentrations between 10-10 M and 10-6 M in a primary rat preputial cell monolayer culture system. Cell growth was determined by number of cells and colonies,and cell differentiation by analysis of lipid-forming colonies. All-trans retinoic acid and selective retinoic acid receptor agonists (CD271 = adapalene,an RAR-beta,gamma agonist; CD2043 = retinoic acid receptor pan-agonist; and CD336 = Am580,an RAR-alpha agonist) caused significant decreases in numbers of cells,colonies,and lipid-forming colonies,but with an exception at high doses of all-trans retinoic acid (10-6 M),with which only a small number of colonies grew but they became twice as differentiated as controls (42.2 +/- 4.0% vs 22.6 +/- 2.7%,mean +/- SEM,lipid-forming colonies,p textless 0.01). Furthermore,the RAR-beta,gamma antagonist CD2665 antagonized the suppressive effects of all-trans retinoic acid,adapalene,and CD2043 on both cell growth and differentiation. In contrast,the retinoid X receptor agonist CD2809 increased cell growth slightly and lipid-forming colonies dramatically in a clear dose-related manner to a maximum of 73.7% +/- 6.7% at 10-6 M (p textless 0. 001). Our data suggest that retinoic acid receptors and retinoid X receptors differ in their roles in sebocyte growth and differentiation: (i) retinoic acid receptors,especially the beta and/or gamma subtypes,mediate both the antiproliferative and antidifferentiative effects of retinoids; (ii) retinoid X receptors mediate prominent differentiative and weak proliferative effects; (iii) the antiproliferative and antidifferentiative effects of all-trans retinoic acid are probably mediated by retinoic acid receptors,whereas its differentiative effect at high dose may be mediated by retinoid X receptors via all-trans retinoic acid metabolism to 9-cis retinoic acid,the natural ligand of retinoid X receptors.
Identification of synthetic retinoids with selectivity for human nuclear retinoic acid receptor gamma.
Biochemical and biophysical research communications 1992 JUL
Abstract
The action of retinoids on gene regulation is mediated by three distinct nuclear retinoic acid receptor (RAR) subtypes called RAR alpha,beta and gamma. Since RAR gamma is predominantly expressed in adult skin,specific ligands for this subtype could (i) represent valuable tools to evaluate the biological role of RAR gamma in skin and (ii) provide therapeutic entities with a higher therapeutic index at lower teratogenic risk. Using in vitro binding studies and a functional transactivation assay,we have identified three compounds with high RAR gamma selectivity.
Dynamic and combinatorial control of gene expression by nuclear retinoic acid receptors (RARs).
Nuclear receptor signaling 2009
Abstract
Nuclear retinoic acid receptors (RARs) are transcriptional regulators controlling the expression of specific subsets of genes in a ligand-dependent manner. The basic mechanism for switching on transcription of cognate target genes involves RAR binding at specific response elements and a network of interactions with coregulatory protein complexes,the assembly of which is directed by the C-terminal ligand-binding domain of RARs. In addition to this scenario,new roles for the N-terminal domain and the ubiquitin-proteasome system recently emerged. Moreover,the functions of RARs are not limited to the regulation of cognate target genes,as they can transrepress other gene pathways. Finally,RARs are also involved in nongenomic biological activities such as the activation of translation and of kinase cascades. Here we will review these mechanisms,focusing on how kinase signaling and the proteasome pathway cooperate to influence the dynamics of RAR transcriptional activity.
更多信息
| 物种 | 人, 其它物种, 大鼠, 小鼠, 非人灵长类 |
|---|---|
| Cas Number | 102121-60-8 |
| Chemical Formula | C₂₂H₂₅NO₃ |
| 纯度 | ≥ 98% |
| Target | RAR |
| Pathway | Retinoid |
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